CN103202842A - 通过用喹喔啉PI3Kα抑制剂抑制来治疗的方法 - Google Patents

通过用喹喔啉PI3Kα抑制剂抑制来治疗的方法 Download PDF

Info

Publication number
CN103202842A
CN103202842A CN2013101161222A CN201310116122A CN103202842A CN 103202842 A CN103202842 A CN 103202842A CN 2013101161222 A CN2013101161222 A CN 2013101161222A CN 201310116122 A CN201310116122 A CN 201310116122A CN 103202842 A CN103202842 A CN 103202842A
Authority
CN
China
Prior art keywords
alkyl
hydrogen
chemotherapeutics
nhc
amino
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
CN2013101161222A
Other languages
English (en)
Chinese (zh)
Inventor
P.兰布
D.马修斯
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Exelixis Inc
Original Assignee
Exelixis Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Exelixis Inc filed Critical Exelixis Inc
Publication of CN103202842A publication Critical patent/CN103202842A/zh
Pending legal-status Critical Current

Links

Images

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/337Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/436Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/498Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/555Heterocyclic compounds containing heavy metals, e.g. hemin, hematin, melarsoprol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN2013101161222A 2007-04-11 2008-04-08 通过用喹喔啉PI3Kα抑制剂抑制来治疗的方法 Pending CN103202842A (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US92316407P 2007-04-11 2007-04-11
US60/923,164 2007-04-11

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CN2008800173944A Division CN101959516B (zh) 2007-04-11 2008-04-08 用以治疗癌症的包含喹喔啉PI3Kα抑制剂的组合治疗

Publications (1)

Publication Number Publication Date
CN103202842A true CN103202842A (zh) 2013-07-17

Family

ID=39864581

Family Applications (2)

Application Number Title Priority Date Filing Date
CN2013101161222A Pending CN103202842A (zh) 2007-04-11 2008-04-08 通过用喹喔啉PI3Kα抑制剂抑制来治疗的方法
CN2008800173944A Expired - Fee Related CN101959516B (zh) 2007-04-11 2008-04-08 用以治疗癌症的包含喹喔啉PI3Kα抑制剂的组合治疗

Family Applications After (1)

Application Number Title Priority Date Filing Date
CN2008800173944A Expired - Fee Related CN101959516B (zh) 2007-04-11 2008-04-08 用以治疗癌症的包含喹喔啉PI3Kα抑制剂的组合治疗

Country Status (33)

Country Link
US (1) US8481001B2 (da)
EP (1) EP2139483B9 (da)
JP (2) JP5726515B2 (da)
KR (1) KR101586774B1 (da)
CN (2) CN103202842A (da)
AU (1) AU2008239668B2 (da)
BR (1) BRPI0810208A2 (da)
CA (1) CA2684056A1 (da)
CO (1) CO6140024A2 (da)
CR (1) CR11099A (da)
CY (1) CY1114608T1 (da)
DK (1) DK2139483T3 (da)
EA (1) EA019064B1 (da)
EC (1) ECSP099723A (da)
ES (1) ES2438998T3 (da)
GT (1) GT200900263A (da)
HR (1) HRP20131081T1 (da)
IL (1) IL201211A (da)
MA (1) MA31335B1 (da)
ME (1) ME00937B (da)
MX (1) MX2009010929A (da)
MY (1) MY150797A (da)
NI (1) NI200900184A (da)
NZ (1) NZ580009A (da)
PL (1) PL2139483T3 (da)
PT (1) PT2139483E (da)
RS (1) RS53020B (da)
SI (1) SI2139483T1 (da)
SV (1) SV2009003390A (da)
TN (1) TN2009000399A1 (da)
UA (1) UA98141C2 (da)
WO (1) WO2008127594A2 (da)
ZA (1) ZA200906765B (da)

Families Citing this family (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BRPI0617162B8 (pt) * 2005-10-07 2021-05-25 Exelixis Inc compostos inibidores de fosfatidilinositol 3-quinase composições farmacêuticas que os contem e métodos de uso dos mesmos
CN101395155A (zh) * 2005-10-07 2009-03-25 埃克塞里艾克西斯公司 PI3Kα的吡啶并嘧啶酮抑制剂
CN101528231A (zh) 2006-08-16 2009-09-09 埃克塞利希斯股份有限公司 在癌症的治疗中使用pi3k和mek调控剂
JP2010523670A (ja) * 2007-04-10 2010-07-15 エクセリクシス, インク. Pi3kアルファのピリドピリミジノン阻害剤を使用した治療方法
WO2010053182A1 (ja) * 2008-11-10 2010-05-14 協和発酵キリン株式会社 キヌレニン産生抑制剤
DE102009049679A1 (de) 2009-10-19 2011-04-21 Merck Patent Gmbh Pyrazolopyrimidinderivate
UY33221A (es) 2010-02-09 2011-09-30 Univ California MÉTODOS PARA TRATAR CÁNCER USANDO INHIBIDORES DE PI3K Y mTOR EN COMBINACIÓN CON INHIBIDORES DE AUTOFAGIA
EP2590654B1 (en) 2010-07-09 2016-12-21 Exelixis, Inc. Combinations of kinase inhibitors for the treatment of cancer
EP2616442B8 (en) 2010-09-14 2018-10-17 Exelixis, Inc. Inhibitors of pi3k-delta and methods of their use and manufacture
BR112013009643A2 (pt) 2010-10-20 2016-07-19 Merck Serono S A Geneva método para preparar n-(3-amino-quinoxalin-2-il)-sulfonamidas substituídas e seus intermediários n-(3-cloo-quinoxalin-2-il)-sulfonamidas
DE102010048800A1 (de) * 2010-10-20 2012-05-10 Merck Patent Gmbh Chinoxalinderivate
DE102010049595A1 (de) 2010-10-26 2012-04-26 Merck Patent Gmbh Chinazolinderivate
WO2012065057A2 (en) 2010-11-12 2012-05-18 Exelixis, Inc. Phosphatidylinositol 3-kinase inhibitors and methods of their use
KR20140077911A (ko) * 2011-09-14 2014-06-24 엑셀리시스, 인코포레이티드 암의 치료를 위한 포스파티딜이노시톨 3-키나아제 저해제
JP2014528451A (ja) * 2011-10-04 2014-10-27 ギリアード カリストガ エルエルシー Pi3kの新規キノキサリン阻害剤
WO2013056067A1 (en) 2011-10-13 2013-04-18 Exelixis, Inc. Compounds for use in the treatment of basal cell carcinoma
KR20140096035A (ko) * 2011-10-28 2014-08-04 노파르티스 아게 위장 기질 종양을 치료하는 방법
CN104302294A (zh) * 2011-11-01 2015-01-21 埃克塞利希斯股份有限公司 用于治疗淋巴组织增生性恶性肿瘤的作为磷脂酰肌醇3-激酶抑制剂的n-(3-{[(3-{[2-氯-5-(甲氧基)苯基]氨基}喹喔啉-2-基)氨基]磺酰基}苯基)-2-甲基丙氨酰胺
WO2013067306A1 (en) * 2011-11-02 2013-05-10 Exelixis, Inc. Phosphatidylinositol 3-kinase inhibitors for the treatment of childhood cancers
CA2860051A1 (en) * 2011-12-27 2013-07-04 Kadmon Corporation, Llc Methods for treatment of breast cancer nonresponsive to trastuzumab
CN103467482B (zh) 2012-04-10 2017-05-10 上海璎黎药业有限公司 稠合嘧啶类化合物,其制备方法,中间体,组合物和应用
WO2014028479A1 (en) 2012-08-13 2014-02-20 Envoy Therapeutics, Inc. Quinoxaline derivatives as gpr6 modulators
US9745321B2 (en) 2013-09-30 2017-08-29 Shanghai Yingli Pharmaceutical Co., Ltd Fused pyrimidine compound, intermediate, preparation method therefor, and composition and application thereof
NZ718487A (en) 2013-10-16 2020-01-31 Shanghai Yingli Pharm Co Ltd Fused heterocyclic compound, preparation method therefor, pharmaceutical composition, and uses thereof
JP6526034B2 (ja) 2014-02-14 2019-06-05 武田薬品工業株式会社 Gpr6のピリドピラジンモジュレーター
US9950194B2 (en) 2014-09-09 2018-04-24 Mevion Medical Systems, Inc. Patient positioning system
WO2019119206A1 (en) * 2017-12-18 2019-06-27 Merck Sharp & Dohme Corp. Purine inhibitors of human phosphatidylinositol 3-kinase delta
WO2023220131A2 (en) * 2022-05-10 2023-11-16 Relay Therapeutics, Inc. PI3Kα INHIBITORS AND METHODS OF USE THEREOF

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004064734A2 (en) * 2003-01-17 2004-08-05 Threshold Pharmaceuticals, Inc. Combination therapies for the treatment of cancer
AU2006283846B2 (en) * 2005-08-26 2012-04-05 Merck Serono Sa Pyrazine derivatives and use as PI3K inhibitors
CN101395155A (zh) 2005-10-07 2009-03-25 埃克塞里艾克西斯公司 PI3Kα的吡啶并嘧啶酮抑制剂
BRPI0617162B8 (pt) 2005-10-07 2021-05-25 Exelixis Inc compostos inibidores de fosfatidilinositol 3-quinase composições farmacêuticas que os contem e métodos de uso dos mesmos
CN101528231A (zh) * 2006-08-16 2009-09-09 埃克塞利希斯股份有限公司 在癌症的治疗中使用pi3k和mek调控剂
NZ578229A (en) * 2007-02-22 2012-02-24 Merck Serono Sa Quinoxaline compounds and use thereof
JP2010523670A (ja) 2007-04-10 2010-07-15 エクセリクシス, インク. Pi3kアルファのピリドピリミジノン阻害剤を使用した治療方法
JP4623164B2 (ja) * 2008-08-21 2011-02-02 セイコーエプソン株式会社 プロジェクタ

Also Published As

Publication number Publication date
EP2139483A2 (en) 2010-01-06
EP2139483B1 (en) 2013-09-18
CA2684056A1 (en) 2008-10-23
RS53020B (sr) 2014-04-30
CY1114608T1 (el) 2016-10-05
NI200900184A (es) 2011-09-08
PL2139483T3 (pl) 2014-02-28
TN2009000399A1 (fr) 2010-12-31
CR11099A (es) 2010-01-19
GT200900263A (es) 2014-01-15
AU2008239668B2 (en) 2013-11-07
MX2009010929A (es) 2010-01-20
ECSP099723A (es) 2010-03-31
ME00937B (me) 2012-06-20
JP2010523669A (ja) 2010-07-15
PT2139483E (pt) 2013-12-27
ZA200906765B (en) 2010-05-26
EA200970935A1 (ru) 2010-04-30
IL201211A0 (en) 2010-05-31
CO6140024A2 (es) 2010-03-19
UA98141C2 (ru) 2012-04-25
SV2009003390A (es) 2010-05-21
JP5726515B2 (ja) 2015-06-03
MY150797A (en) 2014-02-28
CN101959516A (zh) 2011-01-26
EA019064B1 (ru) 2013-12-30
IL201211A (en) 2015-09-24
KR101586774B1 (ko) 2016-01-19
KR20100019436A (ko) 2010-02-18
JP2014074031A (ja) 2014-04-24
DK2139483T3 (da) 2014-01-13
US20110123434A1 (en) 2011-05-26
WO2008127594A3 (en) 2009-04-30
NZ580009A (en) 2012-06-29
HK1140141A1 (en) 2010-10-08
CN101959516B (zh) 2013-05-08
EP2139483B9 (en) 2014-05-21
AU2008239668A1 (en) 2008-10-23
BRPI0810208A2 (pt) 2014-10-21
SI2139483T1 (sl) 2013-11-29
US8481001B2 (en) 2013-07-09
WO2008127594A2 (en) 2008-10-23
MA31335B1 (fr) 2010-04-01
ES2438998T3 (es) 2014-01-21
HRP20131081T1 (hr) 2013-12-20

Similar Documents

Publication Publication Date Title
CN103202842A (zh) 通过用喹喔啉PI3Kα抑制剂抑制来治疗的方法
CN102727498B (zh) 使用吡啶并嘧啶酮PI3Kα抑制剂的治疗方法
EP2056829B9 (en) Using pi3k and mek modulators in treatments of cancer
CN1976906B (zh) 用作parp抑制剂的取代2-烷基喹唑啉酮衍生物
EP1931645B1 (en) N- (3-amino-quinoxalin-2-yl) -sulfonamide derivatives and their use as phosphatidylinositol 3-kinase inhibitors
EP2142543B1 (en) Pyrido [2, 3-d]pyrimidin-7-one compounds as inhibitors of pi3k-alpha for the treatment of cancer
WO2012065057A2 (en) Phosphatidylinositol 3-kinase inhibitors and methods of their use
CN101711249A (zh) 作为PI3K-α的抑制剂用于治疗癌症的吡啶并[2,3-D]嘧啶-7-酮化合物
HK1140141B (en) Combination therapies comprising a quinoxaline inhibitors of pi3k-alpha for use in the treatment of cancer
AU2013201011B2 (en) N- (3-amino-quinoxalin-2-yl) -sulfonamide derivatives and their use as phosphatidylinositol 3-kinase inhibitors
WO2013067306A1 (en) Phosphatidylinositol 3-kinase inhibitors for the treatment of childhood cancers
CN103748095A (zh) 二环杂芳族化合物
HK1139948B (en) Pyrido [2, 3-d]pyrimidin-7-one compounds as inhibitors of pi3k-alpha for the treatment of cancer
HK1162170A (en) N-(3-phenylamino-quinoxalin-2-yl)-benzenesulfonamide derivatives as phosphatidylinositol 3-kinase inhibitors
HK1119697B (en) N- (3-amino-quinoxalin-2-yl) -sulfonamide derivatives and their use as phosphatidylinositol 3-kinase inhibitors
HK1130438B (en) Using pi3k and mek modulators in treatments of cancer

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C02 Deemed withdrawal of patent application after publication (patent law 2001)
WD01 Invention patent application deemed withdrawn after publication

Application publication date: 20130717